2. Protein Tyrosine Kinase/RTK
  3. VEGFR
  4. SAR131675

SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM. SAR131675 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

For research use only. We do not sell to patients.

SAR131675 Chemical Structure

SAR131675 Chemical Structure

CAS No. : 1433953-83-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 94 In-stock
Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Solid
1 mg USD 34 In-stock
5 mg USD 85 In-stock
10 mg USD 140 In-stock
25 mg USD 290 In-stock
50 mg USD 465 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of SAR131675:

SAR131675 Related Antibodies

Top Publications Citing Use of Products

    SAR131675 purchased from MedChemExpress. Usage Cited in: Transl Stroke Res. 2021 Dec;12(6):991-1017.  [Abstract]

    SAR131675 reduces the levels of VEGFR-3, GFAP, neurocan, and phosphacan in astrocytes after OGD/Re with western blotting analysis. Astrocytes are exposed to OGD for 6 h followed by reoxygenation for 24 h. Astrocytes are treated with SAR131675 (20 nM) upon reoxygenation.

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM. SAR131675 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target[1]

    VEGFR3

    23 nM (IC50)

    In Vitro

    AR131675 is highly selective for VEGFR-3. However, it is moderately active on VEGFR-2 with a VEGFR-3/VEGFR-2 ratio of about 10. SAR131675 inhibits VEGFR-3 tyrosine kinase activity and VEGFR-3 autophosphorylation in HEK cells with IC50 values of 20 and 45 nM, respectively. SAR131675 dose dependently inhibits the proliferation of primary human lymphatic cells, induced by the VEGFR-3 ligands VEGFC and VEGFD, with an IC50 of about 20 nM. SSAR131675 has no antiproliferative activity on a panel of 30 tumors and primary cells, further showing its high specificity and indicating that SAR131675 is not a cytotoxic or cytostatic agent[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    SAR131675 Related Antibodies
    In Vivo

    SAR131675 is very well tolerated in mice and shows a potent antitumoral effect in several orthotopic and syngenic models, including mammary 4T1 carcinoma and RIP1.Tag2 tumors. Interestingly, it significantly reduces lymph node invasion and lung metastasis, showing its antilymphangiogenic activity in vivo. SAR131675 significantly reduces TAM infiltration and aggregation in 4T1 tumors[1]. Despite the promising findings, SAR131675 development was terminated during preclinical development due to adverse metabolic effects[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    358.39

    Formula

    C18H22N4O4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C1C(C(NC)=O)=C(N)N(CC)C2=NC(C#C[C@@](COC)(C)O)=CC=C21
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (279.03 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7903 mL 13.9513 mL 27.9026 mL
    5 mM 0.5581 mL 2.7903 mL 5.5805 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.43 mg/mL (3.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.43 mg/mL (3.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (27.90 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.76%

    COA (251 KB) HNMR (146 KB) RP-HPLC (173 KB) LCMS (105 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Multiwell plates are precoated with a synthetic polymer substrate poly-Glu-Tyr (polyGT 4:1). The reaction is carried out in the presence of kinase buffer (10×: 50 mM HEPES buffer, pH 7.4, 20 mM MgCl2, 0.1 mM MnCl2, and 0.2 mM Na3VO4) supplemented with ATP and dimethyl sulfoxide (DMSO) for the positive control (C+) or SAR131675 (ranging from 3-1,000 nM). ATP is used at 30 μM for VEGFR-1 and VEGFR-3 and at 15 μM for VEGFR-2. The phosphorylated poly-GT is probed with a phosphotyrosine specific monoclonal antibody (mAb) conjugated to horseradish peroxidase and developed in the dark with the HRP chromogenic substrate (OPD). The reaction is then stopped by the addition of 100 μL 1.25 mol/L H2SO4, and absorbance is determined using an Envision spectrophotometer at 492 nm[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    HLMVECs are seeded in 96-well plates coated with 0.3% gelatin (5000 cells per well). Cells are incubated in RPMI 0.1% FCS with VEGFA (10 ng/mL) VEGFC (300 ng/mL), VEGFD (300 ng/mL), or FGF2 (10 ng/mL) in the absence or presence of SAR131675. Five days later, viable cells are quantified with the cell Titer-glo luminescent cell viability assay[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mouse: Sterile sponge disks impregnated with 200 μg of FGF2 or PBS are subcutaneously introduced on the back of anaesthetized mice. FGF2 is reinjected into the sponges the first 2 days. Daily oral treatment with SAR131675 (30, 100, and 300 mg/kg/d) started the day of sponge implantation. Seven days later, the animals are euthanatized and the sponges are removed, harvested, and lysed in RIPA buffer at 4°C. After a centrifugation at 6,000 × g, the supernatants are collected for further analysis[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.7903 mL 13.9513 mL 27.9026 mL 69.7564 mL
    5 mM 0.5581 mL 2.7903 mL 5.5805 mL 13.9513 mL
    10 mM 0.2790 mL 1.3951 mL 2.7903 mL 6.9756 mL
    15 mM 0.1860 mL 0.9301 mL 1.8602 mL 4.6504 mL
    20 mM 0.1395 mL 0.6976 mL 1.3951 mL 3.4878 mL
    25 mM 0.1116 mL 0.5581 mL 1.1161 mL 2.7903 mL
    30 mM 0.0930 mL 0.4650 mL 0.9301 mL 2.3252 mL
    40 mM 0.0698 mL 0.3488 mL 0.6976 mL 1.7439 mL
    50 mM 0.0558 mL 0.2790 mL 0.5581 mL 1.3951 mL
    60 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1626 mL
    80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8720 mL
    100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6976 mL
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    SAR131675 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SAR1316751433953-83-3SAR 131675SAR-131675VEGFRVascular endothelial growth factor receptorInhibitorinhibitorinhibit

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